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氨基氰在犬和大鼠体内的药代动力学。

Pharmacokinetics of cyanamide in dog and rat.

作者信息

Obach R, Colom H, Arso J, Peraire C, Pruñonosa J

机构信息

Department of Pharmacology, S.A. LASA Laboratorios, Barcelona, Spain.

出版信息

J Pharm Pharmacol. 1989 Sep;41(9):624-7. doi: 10.1111/j.2042-7158.1989.tb06543.x.

Abstract

A pharmacokinetic study of cyanamide, an inhibitor of aldehyde dehydrogenase (E.C. 1.2.1.3) has been made in the beagle dog and Sprague-Dawley rat. Cyanamide plasma levels were determined by a sensitive high performance liquid chromatographic assay, specific for cyanamide. In the dog, i.v. administration of cyanamide at 1, 2 and 4 mg kg-1, produced a dose-dependent pharmacokinetic behaviour. Statistically significant changes were observed in plasma clearance values (12.6 to 19.7 mL kg-1 min-1), half life values (39 to 61 min) and mean residence times (50 to 79 min). Peak plasma concentrations, after oral administration of 4 mg kg-1 were achieved at 30 min and oral bioavailability was about 65%. In the rat after i.v. or oral administration, cyanamide (2 mg kg-1) had a half life of 30 min, a total plasma clearance of 117 mL kg-1 min-1 and a mean residence time of 26 min. Oral bioavailability was about 69%.

摘要

对醛脱氢酶(E.C. 1.2.1.3)抑制剂氨基氰进行了一项药代动力学研究,实验对象为比格犬和斯普拉格-道利大鼠。氨基氰的血浆水平通过一种对氨基氰具有特异性的灵敏高效液相色谱分析法测定。在犬体内,静脉注射1、2和4 mg kg-1的氨基氰呈现出剂量依赖性药代动力学行为。血浆清除率值(12.6至19.7 mL kg-1 min-1)、半衰期值(39至61分钟)和平均驻留时间(50至79分钟)均观察到具有统计学意义的变化。口服4 mg kg-1后,30分钟达到血浆峰浓度,口服生物利用度约为65%。在大鼠体内,静脉注射或口服2 mg kg-1的氨基氰后,半衰期为30分钟,总血浆清除率为117 mL kg-1 min-1,平均驻留时间为26分钟。口服生物利用度约为69%。

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